title: Pharmacologic activation of p53 by small-molecule MDM2 antagonists.
abstract: Restoring p53 activity by inhibiting the interaction between p53 and MDM2 represents an attractive approach for cancer therapy. To this end, a number of small-molecule p53-MDM2 binding inhibitors have been developed during the past several years. Nutlin-3 is a potent and selective small-molecule MDM2 antagonist that has shown considerable promise in pre-clinical studies. This review will highlight recent advances in the development of small-molecule MDM2 antagonists as potential cancer therapeutics, with special emphasis on Nutlin-3.
authors.affiliation: Department of Anatomy and Cell Biology Rush University Medical Center 1750 W Harrison Ave Jelke Building, Room 1306, USA.
authors.forename: Hong
authors.initials: H
authors.lastname: Shen
authors.forename: Carl G
authors.initials: CG
authors.lastname: Maki
mesh_terms: D000970:Antineoplastic Agents / Q000494:pharmacology*; D016158:Genes, p53; D006801:Humans; D007093:Imidazoles / Q000494:pharmacology*; D058990:Molecular Targeted Therapy; D009369:Neoplasms / Q000188:drug therapy* / Q000378:metabolism; D010879:Piperazines / Q000494:pharmacology*; D011485:Protein Binding; D051736:Proto-Oncogene Proteins c-mdm2 / Q000037:antagonists & inhibitors*; D016159:Tumor Suppressor Protein p53 / Q000819:agonists* / Q000378:metabolism
chemical_list: D000970:Antineoplastic Agents; D007093:Imidazoles; D010879:Piperazines; D016159:Tumor Suppressor Protein p53; C482205:nutlin 3; C497206:MDM2 protein, human; D051736:Proto-Oncogene Proteins c-mdm2